JP2004026816A - Composition for oral cavity - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To obtain a new tablet type composition for applying to the oral cavity, quickly dispersed with saliva when the composition is put in mouth, cleaned by using a teeth brush, or the like, and imparted with excellent feeling in use in the oral cavity by adding a binding agent and a foaming (whipping) agent in a proper ratio. <P>SOLUTION: A sugar alcohol and a disintegrating agent are added to an abrasive, the foaming (whipping) agent, the binding agent and a humectant by combining them in a specific ratio. <P>COPYRIGHT: (C)2004,JPO

Description

【００２３】
表１からも明らかなように、本発明の実施例は比較例に比べ、崩壊性、使用感に優れていた。
【００２４】
実施例４
速崩壊型歯磨
成分　　　　　　　　　　　　　　　　　　　　　　配合量（ｍｇ）
無水ケイ酸　　　　　　　　　　　　　　　　　　　２００
ラウリル硫酸ナトリウム　　　　　　　　　　　　　　１０
キサンタンガム　　　　　　　　　　　　　　　　　　　５
グリセリン　　　　　　　　　　　　　　　　　　　　１０
エリスリトール　　　　　　　　　　　　　　　　　　残部
トレハロース　　　　　　　　　　　　　　　　　　　５０
結晶セルロース　　　　　　　　　　　　　　　　　　５０
塩化セチルピリジニウム　　　　　　　　　　　　　　　０．２５
ステアリン酸マグネシウム　　　　　　　　　　　　　１０
パラベン　　　　　　　　　　　　　　　　　　　　　　５
合計　　　　　　　　　　　　　　　　　　　　　　５００
【００２５】
実施例５
速崩壊型歯磨
成分　　　　　　　　　　　　　　　　　　　　　　配合量（ｍｇ）
リン酸カルシウム　　　　　　　　　　　　　　　　１１５
ラウリル硫酸ナトリウム　　　　　　　　　　　　　　１０
アルギン酸ナトリウム　　　　　　　　　　　　　　　１０
ソルビトール液　　　　　　　　　　　　　　　　　　１５
エリスリトール　　　　　　　　　　　　　　　　　　残部
乳糖　　　　　　　　　　　　　　　　　　　　　　１００
クロスポピドン　　　　　　　　　　　　　　　　　　３０
モノフルオロリン酸ナトリウム　　　　　　　　　　　　３
ステアリン酸マグネシウム　　　　　　　　　　　　　１２
パラベン　　　　　　　　　　　　　　　　　　　　　　５
合計　　　　　　　　　　　　　　　　　　　　　　６００
実施例１に準ずる方法にて製造、６００ｍｇに打錠した。
【００２６】
実施例６
速崩壊型歯磨
成分　　　　　　　　　　　　　　　　　　　　　　配合量（ｍｇ）
炭酸カルシウム　　　　　　　　　　　　　　　　　　８０
ラウリルスルホコハク酸ナトリウム　　　　　　　　１００
カルボキシメチルセルロースナトリウム　　　　　　　１０
グリセリン　　　　　　　　　　　　　　　　　　　　　５
マンニトール　　　　　　　　　　　　　　　　　　　残部
クロスカルメロースナトリウム　　　　　　　　　　　３０
硝酸カリウム　　　　　　　　　　　　　　　　　　　２０
ショ糖脂肪酸ラウリルエステル　　　　　　　　　　　　４
ステアリン酸マグネシウム　　　　　　　　　　　　　１２
パラベン　　　　　　　　　　　　　　　　　　　　　　４
合計　　　　　　　　　　　　　　　　　　　　　　４００
実施例１に準ずる方法にて製造、４００ｍｇに打錠した。
【００２７】
実施例７
速崩壊型歯磨
成分　　　　　　　　　　　　　　　　　　　　　　配合量（ｍｇ）
乳酸菌配合リン酸カルシウム　　　　　　　　　　　１１５
（乳酸菌：Ｌａｃｔｏｂａｃｉｌｌｕｓ　ｓａｌｉｖａｒｉｕｓを１０７ｃｅｌｌ吸着したもの）
アルギン酸ナトリウム　　　　　　　　　　　　　　　１０
ソルビトール液　　　　　　　　　　　　　　　　　　１５
エリスリトール　　　　　　　　　　　　　　　　　　残部
トレハロース　　　　　　　　　　　　　　　　　　１００
クロスポピドン　　　　　　　　　　　　　　　　　　３０
ステアリン酸マグネシウム　　　　　　　　　　　　　１２
合計　　　　　　　　　　　　　　　　　　　　　　６００
【００２８】
実施例４〜７を実施例１と同様の方法にて調製し、１錠あたり６００ｍｇにて、１ｔの負荷にて打錠した。の打錠品を用いて日本薬局方に規定された崩壊試験とパネラー（１０名）による口腔内での崩壊時間の測定を実施した結果、すべて６０秒以内に口腔内で崩壊し、中でも実施例６は４５秒以内に崩壊した。
【００２９】
【発明の効果】
本発明によれば、歯磨成分である研磨剤、発泡剤（起泡剤）、粘結剤及び湿潤剤に糖アルコール及び崩壊剤を適量添加することにより、口腔内において優れた分散性を有しかつ使用感の良い固形型の口腔用組成物が提供できる。[0001]
TECHNICAL FIELD OF THE INVENTION
The present invention relates to a solid oral composition. Further, the present invention relates to maintenance of oral health and the like.
[0002]
[Prior art]
In order to maintain oral health, when brushing teeth, dosage forms such as pastes, liquids, and gels are currently being developed and sold. These dosage forms have changed with the times, and in the old days, powder-shaped toothpastes and powdered toothpastes were mainly used. These have problems in usability and hygiene, and are hardly used except for some tobacco applications. At present, studies on solid dosage forms have hardly been conducted.
[0003]
Solid oral compositions are described, for example, in JP-A-61-236718, JP-A-2-504030, JP-A-4-500368, JP-A-9-87154 and British Patent No. 1259342. It has been disclosed. Japanese Patent Application Laid-Open No. 61-236718 discloses a portable device. The method of use is that of a tablet, which must be chewed and mixed with saliva, and does not disperse quickly in the mouth. In Japanese Patent Application Publication No. 2-504030, it is necessary to chew in the mouth, and there is a problem in use. In Japanese Patent Application Laid-Open No. 4-500368, there is a problem that the hardness of the tablet is increased due to the large amount of powdered sorbitol, and disintegration and dispersibility in the oral cavity are poor. Further, British Patent No. 1259342 discloses a tablet-type dentifrice comprising an abrasive, a detergent, a binder, a surfactant and an oil-adsorbing component, but it can be said that the dentifrice is sufficient in disintegration. The lack was left as a problem.
[0004]
[Patent Document 1]
JP-A-61-236718 [Patent Document 2]
Japanese Patent Publication No. 02-504030 [Patent Document 3]
Japanese Patent Publication No. 04-500368 [Patent Document 4]
Japanese Patent Application Laid-Open No. 09-087154 [Patent Document 5]
British Patent No. 1,259,342
[Problems to be solved by the invention]
Therefore, an object of the present invention is to disperse quickly after putting it in the mouth without using a foaming mechanism such as carbon dioxide at the time of disintegration of the tablet, and to clean it with a toothbrush or the like. It is an object of the present invention to provide a novel tablet-type oral composition having an excellent feeling in use in the oral cavity by adding an appropriate amount of the (foaming agent).
[0006]
[Means for Solving the Problems]
The present inventors have conducted intensive studies to solve the above problems, and as a result, combined a sugar alcohol and a disintegrant in a specific ratio with an abrasive, a foaming agent (foaming agent), a binder and a wetting agent necessary for brushing teeth. As a result, they have found that a tablet-type composition having a fast disintegration property that is excellent in usability when a tablet is put into the oral cavity is obtained, and has completed the present invention.
[0007]
BEST MODE FOR CARRYING OUT THE INVENTION
The solid oral composition of the present invention is excellent in the oral cavity by adding an appropriate amount of a sugar alcohol and a disintegrant to an abrasive, a foaming agent (foaming agent), a binder and a wetting agent, which are dentifrice components. It is intended to provide a solid agent having dispersibility and a good feeling in use. A rapidly disintegrating oral composition refers to one that disintegrates within 60 seconds when contained in the mouth. The time required for disintegration is within 60 seconds, preferably within 45 seconds, more preferably within 30 seconds, even more preferably within 20 seconds.
[0008]
In the present invention, the total amount of the abrasive, foaming agent (foaming agent), binder and wetting agent of the dentifrice component and the total amount of the other components are 1: 0.5 to 1:20 by weight ratio, preferably. The range is from 1: 0.5 to 1:10, most preferably from 1: 1 to 1: 3. If the total amount of components other than the abrasive, the foaming agent (foaming agent), the binder and the wetting agent of the dentifrice component is less than 0.5, there are too few components for forming a tablet, and tableting trouble may occur. When it is generated or a part of the abrasive is used, the hardness increases and a problem arises in disintegration. In addition, when the amount of components other than the abrasive, the foaming agent (foaming agent), the binder and the wetting agent of the dentifrice component exceeds 5, the moldability increases, but a sufficient amount of the dentifrice component may be blended. It is not possible to achieve the purpose as a dentifrice.
[0009]
The sugar or sugar alcohol used in the present invention is not particularly limited to sugar or sugar alcohol, but is preferably lactose, erythritol, xylitol, mannitol, trehalose, sorbitol, maltitol, isomaltitol, palatinose, palatinit, lactitol. And at least one or more are selected and blended.
[0010]
The amount of each component is not particularly limited as long as the moldability and disintegration in the oral cavity are not impaired by the added sugar or sugar alcohol, and is based on the total amount of the oral composition of the present invention. It is preferably from 10 to 70% by weight, more preferably from 30 to 60% by weight. If it is less than 10% by weight, moldability is impaired, and if it exceeds 70% by weight, it is not preferable from the viewpoint of maintaining hardness.
[0011]
The disintegrant used in the present invention is not particularly limited, and is preferably cross-linked polyvinyl pyrrolidone, crystalline cellulose, cellulose and its derivatives, and starch and its derivatives, and at least one is selected from these. The amount of these compounds is preferably 1 to 40% by weight, more preferably 3 to 20% by weight, based on the total amount of the composition of the present invention. If the amount is less than 1% by weight, moldability is impaired, and if it exceeds 40% by weight, moldability is impaired.
[0012]
The abrasive used in the present invention is not particularly limited as long as it is generally used for dentifrices. Calcium hydrogen phosphate, calcium carbonate, aluminum hydroxide, silicic anhydride, silicate, hydroxyapatite, polymethacrylate, metaphosphoric acid Sodium, calcium pyrophosphate and the like are preferred, and at least one or more of these can be blended. The compounding amount of the abrasive component is preferably 5 to 40% by weight, more preferably 10 to 30% by weight, and most preferably 15 to 25% by weight based on the total amount of the composition. If the amount is less than 5% by weight, the effect of cleaning the oral cavity cannot be sufficiently exhibited, and if the amount exceeds 40% by weight, the cleaning effect is not further improved.
[0013]
The foaming agent used in the present invention may be any of an anionic surfactant and a nonionic surfactant which are usually used for dentifrices, and among them, an anionic surfactant is preferable, and sodium lauryl sulfate, sodium myristyl sulfate, and sucrose are particularly preferable. At least one of fatty acid ester, lauroyl sarcosinate and alkyl sulfosuccinate can be blended. The amount of the foaming agent is preferably 0.05 to 30% by weight, more preferably 0.5 to 5% by weight. If the amount is less than 0.05% by weight, the foaming properties are insufficient, and if the amount exceeds 30% by weight, the taste is impaired, which is not preferable.
[0014]
Furthermore, in the present invention, cetylpyridinium chloride, chlorhexidine gluconate, triclosan, isopropylmethylphenol, glycyrrhizin dipotassium, sodium fluoride, sodium monofluorophosphate, casein phosphopeptide, chlorophyll, herbs, tea extract, aluminum lactate, potassium nitrate, lactic acid bacteria, From medicinal agents such as sodium azulene sulfonate, allantoin, cholesterol, sodium chloride, decalinium chloride, ascorbic acid, tocopherol, sodium pyrophosphate, sodium polyphosphate, polyethylene glycol 200-20,000, polyvinylpyrrolidone, lysozyme chloride, hinokitiol, sodium lauroyl sarcosine At least one kind is selected, and its compounding amount is such that the effectiveness is exhibited. The present invention is not limited to.
[0015]
In the present invention, in addition to the above-mentioned components, a binder such as xanthan gum, gum arabic, methylcellulose, sodium carboxymethylcellulose, sodium alginate, guar gum, carrageenan, polyvinyl alcohol, and sodium polyacrylate can be compounded. The amount is preferably 0.1 mg to 50 mg, more preferably 3 to 20 mg.
[0016]
In addition, humectants such as glycerin, sorbitol, propylene glycol, polyethylene glycol, and ethylene glycol can be blended, and the blending amount is preferably 0.1 mg to 100 mg per tablet. Flavoring agents, preservatives, coloring agents, pH adjusters and the like can be added within a range that does not impair the object of the present invention.
[0017]
Further, a lubricant can be added in order to prevent a trouble at the time of tableting, and the method can be used in either the internal lubrication method or the external lubrication method. Flavoring agents are added to provide a refreshing sensation and a refreshing sensation during and after brushing the teeth in order to satisfy the palatability aspects. Specifically, saccharin sodium, dextrose, aspartame, stevia extract, acesulfame, peppermint oil, spearmint oil, eugenol, anethole, spices, etc. are safe, and any physiologically acceptable substances can be blended. It is possible to give a variation to the solid oral composition. Preservatives can be added as long as their safety has been confirmed, such as methyl paraoxybenzoate, butyl paraoxybenzoate, ethyl paraoxybenzoate, and sodium benzoate. The coloring agent can be blended with any coloring agent having a coloring effect mainly on a legal dye. PH adjusters are citric acid and its salts, phosphoric acid and its salts, malic acid and its salts, gluconic acid and its salts, maleic acid and its salts, succinic acid and its salts, glucuronic acid and its salts, fumaric acid and its salts Salts, adipic acid and its salts, lactic acid and its salts, hydrochloric acid, alkali metal hydroxide and the like.
[0018]
The oral composition of the present invention can be provided as a tablet-type toothpaste, tablet confectionery, or supplement, and can be produced by a conventional method.
[0019]
【Example】
Hereinafter, the present invention will be described in more detail with reference to Examples, Comparative Examples, and Test Examples, but the present invention is not limited to these Examples and the like.
[0020]
Examples 1 to 3 and Comparative Examples 1 to 4 shown in Table 1 were prepared and evaluated.
A typical production method will be described. First, calcium phosphate, sodium lauryl sulfate, xanthan gum and the like are well mixed in advance, and a 20% aqueous solution of erythritol is sprayed with a fluid bed granulator and dried sufficiently. Thereafter, erythritol and trehalose are added and mixed well, and then an appropriate amount of water is sprayed and dried to perform granulation. Finally, after adding and mixing microcrystalline cellulose and magnesium stearate, 500 mg is tableted per tablet.
[0021]
Next, the evaluation method will be described.
Disintegration time: It was carried out according to the disintegration test method described in the Japanese Pharmacopoeia, 14th department. The tester was attached to a receiving shaft, placed in a beaker, and reciprocated 30 times for 1 minute, and moved up and down at an amplitude of 55 mm to perform a test. Water was used as the test solution, and the temperature was 37 ° C.
◎: Within 45 seconds, ：: Within 60 seconds, ×: Disintegration time exceeding 60 seconds Disintegration time (in the oral cavity):
◎: Within 45 seconds, ：: Within 60 seconds, ×: Disintegration time exceeding 60 seconds Amount of saliva:
：: Saliva does not overflow from the mouth, ×: Foaming with a feeling that saliva seems to overflow from the mouth: The preparation was contained in the mouth, brushed after disintegration, and the degree of foaming was evaluated.
：: Foaming that does not cause any problem in actual use is obtained. X: Foaming is insufficient or foaming is not evaluated.
A: The disintegration time (in the oral cavity) is ◎, and X is not included. B: Each evaluation item is ○, and C is not included, C: Includes X.
[Table 1]

[0023]
As is evident from Table 1, the examples of the present invention were superior to the comparative examples in disintegration and feeling in use.
[0024]
Example 4
Fast-disintegrating dentifrice ingredients (mg)
Silicic anhydride 200
Sodium lauryl sulfate 10
Xanthan gum 5
Glycerin 10
Erythritol balance trehalose 50
Crystalline cellulose 50
Cetylpyridinium chloride 0.25
Magnesium stearate 10
Paraben 5
500 in total
[0025]
Example 5
Fast-disintegrating dentifrice ingredients (mg)
Calcium phosphate 115
Sodium lauryl sulfate 10
Sodium alginate 10
Sorbitol solution 15
Erythritol balance lactose 100
Crospopidone 30
Sodium monofluorophosphate 3
Magnesium stearate 12
Paraben 5
Total 600
Manufactured by the method according to Example 1, and tableted to 600 mg.
[0026]
Example 6
Fast-disintegrating dentifrice ingredients (mg)
Calcium carbonate 80
Sodium lauryl sulfosuccinate 100
Sodium carboxymethylcellulose 10
Glycerin 5
Mannitol balance croscarmellose sodium 30
Potassium nitrate 20
Sucrose fatty acid lauryl ester 4
Magnesium stearate 12
Paraben 4
400 in total
Manufactured by the method according to Example 1, and tableted to 400 mg.
[0027]
Example 7
Fast-disintegrating dentifrice ingredients (mg)
Calcium phosphate containing lactic acid bacteria 115
(Lactobacillus: Lactobacillus salivarius adsorbed by 107 cells)
Sodium alginate 10
Sorbitol solution 15
Erythritol balance trehalose 100
Crospopidone 30
Magnesium stearate 12
Total 600
[0028]
Examples 4 to 7 were prepared in the same manner as in Example 1, and tableted at a load of 1 t at 600 mg per tablet. As a result of the disintegration test prescribed by the Japanese Pharmacopoeia and the measurement of the disintegration time in the oral cavity by panelists (10 persons) using the tableted product, all disintegrated in the oral cavity within 60 seconds. 6 collapsed within 45 seconds.
[0029]
【The invention's effect】
ADVANTAGE OF THE INVENTION According to this invention, it has excellent dispersibility in an oral cavity by adding a sugar alcohol and a disintegrating agent to the dentifrice component of the abrasive, the foaming agent (foaming agent), the binder and the wetting agent in an appropriate amount. In addition, a solid oral composition having a good feeling in use can be provided.

Claims (7)

A tablet containing sugar or sugar alcohol, a disintegrant, an abrasive, a foaming agent, a binder and a wetting agent, wherein the total amount of the abrasive, foaming agent, binder and wetting agent and other components A rapidly disintegrating oral composition, wherein the composition ratio is in the range of 1: 0.5 to 1:20. A tablet containing sugar or sugar alcohol, a disintegrant, an abrasive, a foaming agent, a binder and a wetting agent, wherein the total amount of the abrasive, foaming agent, binder and wetting agent and other components A rapidly disintegrating oral composition, wherein the composition ratio is in the range of 1: 0.5 to 1:10. The sugar or sugar alcohol is one or more kinds selected from lactose, erythritol, xylitol, mannitol, trehalose, sorbitol, maltitol, isomaltitol, palatinose, palatinit, lactitol. Oral composition. The oral composition according to any one of claims 1 to 3, wherein the disintegrant is at least one selected from crosslinked polyvinylpyrrolidone, crystalline cellulose, cellulose and derivatives thereof, and starch and derivatives thereof. The abrasive is at least one selected from the group consisting of calcium hydrogen phosphate, calcium carbonate, aluminum hydroxide, silicic anhydride, silicate, hydroxyapatite, polymethacrylate, sodium metaphosphate and calcium pyrophosphate. The composition for oral cavity according to any one of claims 4 and 4. The foaming agent is at least one selected from the group consisting of sodium lauryl sulfate, sodium myristyl sulfate, sucrose fatty acid ester, lauroyl sarcosinate, and lauryl sulfosuccinate. The oral composition according to item. In addition, cetylpyridinium chloride, chlorhexidine gluconate, triclosan, isopropylmethylphenol, dipotassium glycyrrhizin, sodium fluoride, sodium monofluorophosphate, casein phosphopeptide, chlorophyll, herbs, tea extract, aluminum lactate, potassium nitrate, lactic acid bacteria, sodium azulene sulfonate Selected from allantoin, cholesterol, sodium chloride, decalinium chloride, ascorbic acid, tocopherol, sodium pyrophosphate, sodium polyphosphate, polyethylene glycol (average molecular weight 200 to 20,000), polyvinylpyrrolidone, lysozyme chloride, hinokitiol, lauroyl sarcosine sodium, lactoferrin 7. The method according to claim 1, wherein at least one kind is compounded. Oral composition according to item.